October 2018 - Corcept Therapeutics

A mixed glucocorticoid/mineralocorticoid selective modulator with dominant antagonism in the male rat brain.

October 25, 2018

Atucha et al. • 2015 • Endocrinology. 2015;156(11):4105-4114.

Identification of the clinical candidate (R)-(1-(4-Fluorophenyl)-6-((1-methyl-1H-pyrazol-4-yl)sulfonyl)-4,4a,5,6,7,8-hexahydro-1H-pyrazolo[3,4-g]isoquinolin-4a-yl)(4-(trifluoromethyl)pyridin-2-yl)methanone (CORT125134): a selective Glucocorticoid Receptor (GR) antagonist.

October 25, 2018

Hunt et al. • 2017 • J Med Chem. 2017;60(8):3405-3421.

1H-pyrazolo[3,4-g]hexahydro-isoquinolines as selective glucocorticoidreceptor antagonists with high functional activity.

October 25, 2018

Clark et al. • 2008 • Bioorg Med Chem Lett. 2008;18(4):1312-7.

Assessment of safety, tolerability, pharmacokinetics, and pharmacological effect of orally administered CORT125134: an adaptive, double-blind, randomized, placebo-controlled phase 1 clinical study.

October 25, 2018

Hunt et al. • 2017 • Clin Pharmacol Drug Dev. 2017 Oct 2. doi: 10.1002/cpdd.389.

FKBP5 mRNA expression is a biomarker for GR antagonism.

October 25, 2018

Bali et al. • 2016 • J Clin Endocrinol Metab. 2016;101(11):4305-4312.

Selective Glucocorticoid Receptor Modulators (SGRMs) delay castrate-resistant prostate cancer growth.

October 18, 2018

Kach et al. • 2017 • Mol Cancer Ther. 2017;16(8):1680-1692.